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Steroidal CYP inhibitors can further be classified based on
2024-01-19
Steroidal CYP17 inhibitors can further be classified based on their mode of action, namely as mechanism-based inhibitors and type I and type II competitive inhibitors [129]. Recent studies investigated other biological targets than CYP17, and some new compounds have shown interesting dual activity a
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br The role of cytochrome b with cytochrome
2024-01-19
The role of cytochrome b5 with cytochrome P450 17α-hydroxylase/17,20-lyase Conclusion Acknowledgments LLM and RJR wish to thank the Australian Research Council and the National Health and Medical Research Council of Australia for funding. The problem One area of modern medicine that con
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Taking together findings from our study and that
2024-01-19
Taking together findings from our study and that from the literature, we propose a model (to be experimentally confirmed) of possible intracellular mechanism of NA-induced regulation of Na-K ATPase subunit expression (Fig. 8). NA acting on α1-AR modulates the α1- and α3-subunit expressions of Na-K A
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br Introduction Lung cancer is the leading cause of cancer
2024-01-19
Introduction Lung cancer is the leading cause of cancer death worldwide and is one of the most refractory of solid tumors along with pancreatic cancer. Since 1975 there have been notable improvements in the 5-year survival rate of patients with lung cancer [1]. This improvement in survival is tho
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br Experimental br Results and discussion br
2024-01-19
Experimental Results and discussion Conclusion Acknowledgments This work is supported by the National Basic Research Program of China (973 Program 2016YFA0201201 and 2013CB932702), a project funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions (PAP
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It is now thought that
2024-01-18
It is now thought that tight binding of HMGB to condensed chromatin may not be restricted to apoptotic cells. That HMGB proteins might actually be involved in the organization and/or maintenance of heterochromatic regions is suggested by the results of experiments analyzing the stable binding of the
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br Materials and methods br Results In order to eval
2024-01-18
Materials and methods Results In order to evaluate changes in the amount of PKC-θ expressed by MEL cells at different stages of the cell cycle, we measured the level of the kinase in cells collected from cultures containing 90% of cells in the interphase or 80% cells synchronized at the metaph
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On the other hand oxygen concentration in
2024-01-18
On the other hand, oxygen concentration in tumor tissue also depends on its consumption rate by tumor cells, which decrease will also lead to alleviation of hypoxia. This fact is not taken into account in the majority of studies on the topic, although it is well-known that antiangiogenic therapy doe
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ERAP has been crystallized in two
2024-01-18
ERAP1 has been crystallized in two different conformations, wherein the C-terminal domain IV is either closely interacting with domains I/II and enclosing the active site (termed ‘closed’), or is rotated away in a hinge motion which exposes the active site (‘open’). This large motion correlates with
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Through an extensive SAR optimization
2024-01-18
Through an extensive SAR optimization campaign with the 4-((2-hydroxy-3-methoxybenzyl)amino)-benzenesulfonamide-based scaffold researchers have developed ML355 ((N-benzo[d]thiazol-2-yl)-4((2-hydroxy-3 methoxybenzyl)amino)benzenesulfonamide) [5]. ML355 is a nonreductive, noncompetitive, reversible 12
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In conclusion we have shown that mGlu
2024-01-18
In conclusion, we have shown that mGlu7 receptors negatively regulate α1-adrenergic receptor signalling in heterologous expression systems, T7 High Yield Cy3 RNA tissue and living animals. This interaction might represent a protective mechanism aimed at restraining an excessive activation of noradr
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Endogenous adenosine systems have largely been implicated in
2024-01-18
Endogenous adenosine systems have largely been implicated in drug actions by the demonstration that caffeine (non-selective A1R and A2AR antagonist) (see Section The issue of caffeine), in doses up to 7.5–10mg/kg, inhibits antinociception, and when this occurs, it AG-14361 receptor is generally als
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In the past years the role of
2024-01-18
In the past 10 years, the role of the CD73-adenosinergic pathway in suppression of anti-tumor immunity has increasingly been recognized [13], [14]. In this review, we discuss the latest findings dealing with the regulation of anti-tumor immunity by CD73 and adenosine. We also discuss ongoing clinica
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We aim to evaluate the AK in
2024-01-18
We aim to evaluate the AK in regulating adenosine signaling in the retina. It was reported that the degree of Chidamide injury directly depends on expression levels of AK and the resulting extracellular levels of adenosine (Boison, 2006). Indeed, transgenic mice overexpressing AK are highly suscept
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br Conflict of interest br Acknowledgments This work
2024-01-18
Conflict of interest Acknowledgments This work was supported by research grant [PR26/20326] from Santander Bank/UCM. The authors would like to thank Miguel Capo, Professor of Toxicology from the Universidad Complutense de Madrid, for his counseling during the preparation of the present work.
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